Caffeine in tablets - for weight loss

In the instruction indications for the use of caffeine in diet pills are absent: this purine methylxanthine alkaloid belongs to the group of psychostimulating substances affecting the central nervous system.

The caffeine names used are: 1,3,7-trimethyl-xanthine (chemical); caffeine-benzoate sodium or caffeine sodiumbenzoate (pharmaceutical); alternative - methylteobromine, theine, guaranine.

[1], [2], [3], [4]

Indications of the caffeine in diet pills

Indications for use of sodium caffeine-benzoate cover the spectrum of diseases of the central nervous and cardiovascular systems with spasms, decreased vascular tone and blood pressure, as well as narcolepsy and asthenic conditions with increased fatigue, drowsiness and a general decline in strength.

In addition, sodium caffeine-benzoate (caffeine in tablets) has been used to reduce body weight, since its mechanism of action extends not only to certain functions of the autonomic nervous system, but also to metabolic processes that - with the help of neurotransmitters (transmitting chemical impulses) - the brain controls.

Release form

Form release caffeine-benzoate sodium tablets, powder, solution for injection (10 and 20%) in ampoules.

[5], [6], [7], [8]

Pharmacodynamics

Pharmacodynamics: How Caffeine Helps Burn Fat

The mechanism of action, that is, the pharmacodynamics of sodium caffeine-benzoate, is based on several biochemical processes. First, caffeine depresses the effector cell enzyme phosphodiesterase, which regulates the transfer of intracellular signals, and this is reflected in an increase in the concentration of the cAMP-cyclic adenosine monophosphate generating hormone. As a result, cAMP increases the activity of fat cell enzymes (adipocytes) that break down triglycerides, and thus the intensity of lipolysis in cells of visceral adipose tissue increases.

An important role is played by the similarity of the chemical structure of caffeine (the methylated purine base of xanthine) to the molecular structure of the adenosine produced by the body, a purine neurotransmitter that inhibits brain excitation. Molecules of caffeine can bind to adenosine receptors in brain cells and do not allow them to activate, that is, they act as a competitive antagonist. But for the fat burning process, the key is that this antagonism promotes the release and activation of catecholamine neurotransmitters, including adrenaline.

Adrenaline acts on membrane adrenoreceptors of adipose tissue cells and also stimulates enzymes involved in the cleavage of triglycerides.

In addition, the effect of caffeine in diet pills is associated with its diuretic effect, which arises from the inhibition of water reabsorption in the renal tubules. However, an increase in the volume of urine is observed only with a dose of caffeine of more than 300 mg.

Caffeine, like most psychostimulants, suppresses appetite, that is, delays the signal of hunger, but the mechanism of this effect is not yet known.

[9], [10], [11], [12], [13]

Pharmacokinetics

Caffeine-sodium benzoate is well absorbed in the digestive tract (within 30-45 minutes), enters the systemic circulation (the connection with serum proteins does not exceed 15%) and is distributed in tissues and interstitial fluids; penetrates through the BBB.

More than 90% of caffeine is metabolized by the enzymatic system of the liver by demethylation and oxidation to active and inactive metabolites. Among the primary active dimethylxanthines, paraxanthin plays a special role in the activation of lipolysis, and the content of glycerol and free fatty acids increases in blood plasma.

The drug is not cumulated. The half-life of the biotransformation products of sodium caffeine-benzoate averages 4.5-6 hours; excretion - through the kidneys (with urine) and through the intestines (with feces).

[14], [15], [16], [17], [18]

Dosing and administration

Caffeine in diet pills is taken orally, but there are different approaches to its dosage.

According to one recommendation, it is necessary to take 100 mg for every 30 kg of body weight, and only before physical training (for 40-45 minutes); others argue that the optimal dose is 10-20 mg per kilogram of body weight.

Some sources indicate the maximum single dose of caffeine in tablets - 400 mg, and daily - 1 g.

Specialists of the American Medical Association consider a moderate dose of caffeine 200-300 mg per day. Half of this amount is recommended to take a quarter of an hour before breakfast (thereby reducing the appetite for at least half a day), the second reception - 15-20 minutes before lunch (but no later than 16 hours).

[25], [26], [27], [28], [29], [30]

Use of the caffeine in diet pills during pregnancy

Caffeine penetrates the placenta and enters the breast milk; for this reason, its use during pregnancy and during lactation is contraindicated.

Contraindications

Sodium caffeine-benzoate is contraindicated if there is a history of hypersensitivity to caffeine, hyperexcitability of the central nervous system, epilepsy, cardiovascular pathologies of an organic nature, myocardial infarction, tachycardia, arterial hypertension, chronic insomnia, glaucoma. The drug is not used in the elderly and children under 12 years of age.

[19], [20], [21], [22]

Side effects of the caffeine in diet pills

The main side effects of caffeine in tablets are expressed in the form of nervousness, tremor, headache, sleep disorders, cardiac arrhythmia, increased blood pressure, nausea, pain in the epigastric region. Allergic reactions with urticaria and skin pruritus are possible.

A significant increase in diuresis can lead to dehydration of the body. Also, with prolonged use of sodium caffeine-benzoate, there is a risk of dependence - caffeine. And with a sharp discontinuation of reception may increase drowsiness and depressive stagnation.

[23], [24]

Overdose

Excess dosage of sodium caffeine-benzoate leads to pain in the stomach, nausea, vomiting, nervous overexcitation, increased heart rate, heat, tremor and convulsions.

In case of overdosage, it is necessary to wash the stomach, take activated charcoal: with convulsions, intravenous injections of anticonvulsants, in particular benzodiazepines, are made.

[31], [32]

Interactions with other drugs

Caffeine-sodium benzoate enhances the action of analgesics (not opioid), antipyretic agents, alpha and beta-adrenomimetics, thyreotropic drugs.

Caffeine reduces the effect of tranquilizers, opioid analgesics, soothing and hypnotic drugs.

Enhance the effects of caffeine for hormonal contraception; antibiotics slow down the elimination of caffeine and increase its concentration in the blood plasma.

The use of caffeine concurrent with cardiac glycosides increases not only their therapeutic effect, but also side effects.

Caffeine is absolutely incompatible with the drugs that depress the central nervous system, in particular, drugs for general anesthesia.

[33], [34], [35], [36], [37]

Storage conditions

Caffeine-sodium benzoate should be stored at room temperature, in a place inaccessible to children.

[38], [39], [40], [41], [42]

Shelf life

Shelf life of the drug is 4 years.

Reviews

The real opinions of those who lose weight and the results are not published in accessible sources, obviously, due to the fact that sodium caffeine-benzoate is not advertised by the pharmaceutical enterprises that produce it.

A few reviews of doctors are reduced to the fact that caffeine can slightly reduce body weight or prevent it from increasing, but "there is no convincing evidence that caffeine causes significant or permanent weight loss."